Patent RU-2293728-C2 (RU)
Inventor: BEK DZHEJMS P
IPC: A61P25/28
Filed: 2000-11-03
Granted: 2007-02-20
Abstract: FIELD: organic chemistry, medicine, pharmacy. 
     SUBSTANCE: invention relates to novel tetrahydroisoquinolines that are useful in treatment of different neurological and psychic disorders, for example, ADHD. Invention describes a derivative of tetrahydroisoquinoline represented by the formula (IA-IF):   wherein carbon atom designated as * is in R- or S-configuration; R 1  represents (C 1 -C 6 )-alkyl; R 2  represents hydrogen atom (H), (C 1 -C 6 )-alkyl; R 3  represents H, -S(O) n NR 11 R 12 , (C 1 -C 6 )-alkyl or if R represents (C 1 -C 6 )-alkyl then the indicated group is substituted optionally with 1-3 substitutes chosen independently from the following groups in each case: (C 1 -C 6 )-alkyl, -OR 9  and -NR 9 R 10  under condition that in compounds represented by the formula (IA) radical R 3  represents (C 1 -C 6 )-alkyl that is substituted optionally with 1-3 substitutes chosen independently among the following groups in each case: (C 1 -C 6 )-alkyl, -OR 9  and -NR 9 R 10 ; R 4  represents H, (C 1 -C 6 )-alkyl, and when R 4  represents (C 1 -C 6 )-alkyl then indicated group is substituted optionally with 1-3 substitutes chosen independently from the following groups in each case: (C 1 -C 3 )-alkyl, halogen atom, -OR 9  and -NR 9 R 10  under condition that in compounds represented by the formula (ID) radical R 4  represents (C 1 -C 6 )-alkyl that is optionally substituted, and wherein both R 3  and R are not hydrogen atom; each R 5 , R 6  and R 7  in compounds represented by each formula (IA), (IB), (IC), (ID), (IE) and (IF) represents independently H, halogen atom, -OR 11 , -NR 11 C(O)R 12  and (C 1 -C 6 )-alkyl, and when each radical among R 5 , R 6  and R 7  represents (C 1 -C 6 )-alkyl then indicated group is substituted optionally with 1-3 substitutes chosen independently in each case from the following groups: (C 1 -C 3 )-alkyl, halogen atom under condition that in compounds represented by the formula (IE) at least one radical among R 5  or R 7  represents fluorine, chlorine atom or methyl group; R 8  represents H or halogen atom under condition that in compounds represented by the formula (IF) radical R represents halogen atom; each R 9  and R 10  represents independently H, (C 1 -C 4 )-alkyl; R 11  represents H, (C 1 -C 4 )-alkyl, and when R 11  represents (C 1 -C 4 )-alkyl then indicated group is substituted optionally with 1-3 substitutes chosen independently in each case from the following groups: halogen atom, (C 1 -C 4 )-alkyl; R 12  represents H, (C 1 -C 4 )-alkyl; n = 2, and its pharmaceutically acceptable salt or solvate. Also, invention describes a pharmaceutical composition, a method for treatment of disorder caused or associated with deficiency in serotonin, noradrenaline or dopamine, a method for inhibition of synaptic uptake of noradrenaline, a method for inhibition of synaptic uptake of serotonin, a method for inhibition of synaptic uptake of dopamine and a set comprising, among them, a compound by cl. 1. Invention provides synthesis of novel compounds possessing the useful biological properties. 
     EFFECT: valuable medicinal properties of compounds and pharmaceutical composition, improved method of treatment and inhibition. 
     44 cl, 5 tbl, 94 ex